Pharmacology Unit, Department of Biomedical Sciences, School of Medicine and Health Sciences, Universidad del Rosario, Bogotá 111221, Colombia.
GENIUROS Research Group, Center for Research in Genetics and Genomics (CIGGUR), School of Medicine and Health Sciences, Universidad del Rosario, Bogotá 111221, Colombia.
Int J Mol Sci. 2022 Sep 5;23(17):10190. doi: 10.3390/ijms231710190.
The solubility of drugs in cosolvent systems of pharmaceutical interest is of great importance for understanding and optimizing a large number of processes. Here, we report the solubility of isoniazid in nine (PEG 200 + water) cosolvent mixtures at nine temperatures (278.15, 283.15, 288.15, 293.15, 298.15, 303.15, 308.15, and 318.15 K) determined by UV-vis spectrophotometry. From the solubility data, the thermodynamic solution, mixing, and transfer functions were calculated in addition to performing the enthalpy-entropy compensation analysis. The solubility of isoniazid depends on the concentration of PEG 200 (positive cosolvent effect) and temperature (endothermic process) reaching its maximum solubility in pure PEG 200 at 318.15 K and the lowest solubility in pure water at 278.15 K. The solution process is favored by the solution entropy and according to the enthalpy-entropy compensation analysis it is driven by entropy in mixtures rich in water and by enthalpy in mixtures rich in PEG 200.
药物在具有药用兴趣的共溶剂体系中的溶解度对于理解和优化大量过程非常重要。在这里,我们报告了异烟肼在九种(PEG 200 + 水)共溶剂混合物中的溶解度,在九个温度(278.15、283.15、288.15、293.15、298.15、303.15、308.15 和 318.15 K)下通过紫外可见分光光度法测定。从溶解度数据中,除了进行焓熵补偿分析外,还计算了热力学溶液、混合和传递函数。异烟肼的溶解度取决于 PEG 200 的浓度(正共溶剂效应)和温度(吸热过程),在 318.15 K 的纯 PEG 200 中达到最大溶解度,在 278.15 K 的纯水中达到最低溶解度。溶液过程有利于溶液熵,并且根据焓熵补偿分析,它在富含水的混合物中由熵驱动,在富含 PEG 200 的混合物中由焓驱动。